Azole compounds endowed with antimycotic activity for human...

C - Chemistry – Metallurgy – 07 – D

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C07D 249/08 (2006.01) A61K 31/41 (2006.01) C07D 233/60 (2006.01) C07D 521/00 (2006.01) C12P 17/10 (2006.01) C12P 41/00 (2006.01)

Patent

CA 2247390

Compounds of formula (II-A) wherein R1 is chloro, fluoro, bromo or trifluoromethyl; R2 is hydrogen, chloro, fluoro, bromo or trifluoromethyl; Z is CH or N; R3, R4 and R5, which are the same or different, are hydrogen or C1- C4 alkyl, with the proviso that R4 is different from R5 when R3 is hydrogen; X is O, S, SO or SO2; R6 is a C1-C5 polyfluoroalkyl group containing at least two fluorine atoms and optionally other halogen atoms selected from the group consisting of chloro and bromo; processes for their preparation and pharmaceutical compositions containing them are described. The compounds of formula (II-A) are endowed with a marked wide range antimycotic activity.

L'invention concerne des composés de formule (II-A). Dans cette formule, R¿1? est un groupe chloro, fluoro, bromo ou trifluorométhyle; R¿2? est un hydrogène, chloro, fluoro, bromo ou trifluorométhyle: Z est CH ou N; R¿3?, R¿4? et R¿5?, qui peuvent être les mêmes ou différents, sont l'hydrogène ou un C¿1-4?alkyle, à condition que R¿4? soit différent de R¿5? quand R¿3? est un hydrogène; X est O, S, SO ou SO¿2?; R¿6? est un groupe C¿1?-C¿5?polyfluoroalkyle contenant au moins deux atomes de fluor et éventuellement d'autres atomes d'halogène, choisis dans le groupe constitué par chloro et bromo. L'invention concerne également des procédés de préparation de ces composés et des compositions pharmaceutique les contenant. Les composés de la formule (II-A) ont un spectre d'activité antimycotique très large.

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